ArticleChemistry (Weinheim an der Bergstrasse, Germany)2014
Redesigning the DNA-targeted chromophore in platinum-acridine anticancer agents: a structure-activity relationship study.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 56 citations in OpenAlex.
- A state-of-the-art view: G-quadruplex-targeting for platinum complexes' treatment of tumors.RSC chemical biology · 2025Review
- An Overview of Acridine Analogs: Pharmacological Significance and Recent Developments.Current medicinal chemistry · 2025Review
- A CD Study of a Structure-Based Selection ofMolecules (Basel, Switzerland) · 2024Article
- Platinum-Acridine Agents with High Activity in Cancers Expressing the Solute Carrier MATE1 (ACS medicinal chemistry letters · 2023Article
- Acridine as an Anti-Tumour Agent: A Critical Review.Molecules (Basel, Switzerland) · 2022Review
- Computational and Experimental Characterization of rDNA and rRNA G-Quadruplexes.The journal of physical chemistry. B · 2022Article
- DNA Adduct Detection after Post-Labeling Technique with PCR Amplification (DNA-ADAPT-qPCR) Identifies the Pre-ribosomal RNA Gene as a Direct Target of Platinum-Acridine Anticancer Agents.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Metal-Based G-Quadruplex Binders for Cancer Theranostics.Pharmaceuticals (Basel, Switzerland) · 2021Review
- A DNA small molecular probe with increasing KRSC advances · 2021Article
- Evaluation of a Platinum-Acridine Anticancer Agent and Its Liposomal Formulation in an in vivo Model of Lung Adenocarcinoma.ChemMedChem · 2021Article
- Synthesis and biological evaluation of 2-phenyl-4-aminoquinolines as potential antifungal agents.Molecular diversity · 2020Article
- Thermodynamic Insights by Microscale Thermophoresis into Translesion DNA Synthesis Catalyzed by DNA Polymerases Across a Lesion of Antitumor Platinum-Acridine Complex.International journal of molecular sciences · 2020Article
- Human Serum Albumin-Delivered [Au(PEtACS medicinal chemistry letters · 2017Article
- Large-Pore Functionalized Mesoporous Silica Nanoparticles as Drug Delivery Vector for a Highly Cytotoxic Hybrid Platinum-Acridine Anticancer Agent.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Synthesis and antitumor mechanism of a new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol as ligands.MedChemComm · 2017Article
- Design and cellular studies of a carbon nanotube-based delivery system for a hybrid platinum-acridine anticancer agent.Journal of inorganic biochemistry · 2016Article
- Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity.Scientific reports · 2016Article
- Transition Metal Intercalators as Anticancer Agents-Recent Advances.International journal of molecular sciences · 2016Review
- Linker design for the modular assembly of multifunctional and targeted platinum(ii)-containing anticancer agents.Dalton transactions (Cambridge, England : 2003) · 2016Article
- Chromatin folding and DNA replication inhibition mediated by a highly antitumor-active tetrazolato-bridged dinuclear platinum(II) complex.Scientific reports · 2016Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
Platinum-acridine hybrid agents show low-nanomolar potency in chemoresistant non-small cell lung cancer (NSCLC), but high systemic toxicity in vivo. To reduce the promiscuous genotoxicity of these agents and improve their pharmacological properties, a modular build-click-screen approach was used to evaluate a small library of twenty hybrid agents containing truncated and extended chromophores of varying basicities. Selected derivatives were resynthesized and tested in five NSCLC cell lines representing large cell, squamous cell, and adenocarcinomas. 7-Aminobenz[c]acridine was identified as a promising scaffold in a hybrid agent (P1-B1) that maintained submicromolar activity in several of the DNA-repair proficient and p53-mutant cancer models, while showing improved tolerability in mice by 32-fold compared to the parent platinum-acridine (P1-A1). The distribution and DNA/RNA adduct levels produced by the acridine- and benz[c]acridine-based analogues in NCI-H460 cells (confocal microscopy, ICP-MS), and their ability to bind G-quadruplex forming DNA sequences (CD spectroscopy, HR-ESMS) were studied. P1-B1 emerges as a less genotoxic, more tolerable, and potentially more target-selective hybrid agent than P1-A1.
Indexed as
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.